Cytotoxic Activity of Some Natural and Synthetic ent-Kauranes

Atractyligenin (1) and several synthetic derivatives were tested and found to be active against tumor cell replication. Compound 1 was readily converted to the 2,15-diketo (3) or 15-keto (4) derivatives, which contain an α,β-unsaturated ketone. Compounds 3 and 4 showed significant cytotoxic activity...

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Veröffentlicht in:	Journal of natural products (Washington, D.C.) D.C.), 2007-03, Vol.70 (3), p.347-352
Hauptverfasser:	Rosselli, Sergio, Bruno, Maurizio, Maggio, Antonella, Bellone, Gabriella, Chen, Tzu-Hsuan, Bastow, Kenneth F, Lee, Kuo-Hsiung
Format:	Artikel
Sprache:	eng
Schlagworte:	anticarcinogenic activity Antineoplastic agents Antineoplastic Agents, Phytogenic - chemical synthesis Antineoplastic Agents, Phytogenic - isolation & purification Antineoplastic Agents, Phytogenic - pharmacology Asteraceae Asteraceae - chemistry atractyligenin Atractyloside - analogs & derivatives Atractyloside - pharmacology Biological and medical sciences Chamaeleon gummifer cultured cells cytotoxicity Diterpenes, Kaurane - chemical synthesis Diterpenes, Kaurane - isolation & purification Diterpenes, Kaurane - pharmacology diterpenoids Drug Screening Assays, Antitumor esters Female General aspects Humans kaurane diterpene ketones Lamiaceae - chemistry Medical sciences Molecular Structure Ovarian Neoplasms Pharmacology. Drug treatments phytochemicals Plants, Medicinal - chemistry Tumor Cells, Cultured
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Beschreibung
Zusammenfassung:	Atractyligenin (1) and several synthetic derivatives were tested and found to be active against tumor cell replication. Compound 1 was readily converted to the 2,15-diketo (3) or 15-keto (4) derivatives, which contain an α,β-unsaturated ketone. Compounds 3 and 4 showed significant cytotoxic activity against all six tested cancer cell lines and were most potent against 1A9 ovarian cancer cells with EC50 values of 0.2 and 0.3 μM, respectively. These two 1-analogues are promising lead compounds for further investigation.
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np060504w